BGB-43395 / BeOne Medicines - LARVOL DELTA

BGB-43395-103: A Study of Different Forms of BGB-43395 and Food Effect in Healthy Participants (clinicaltrials.gov) - P1 | N=51 | Completed | Sponsor: BeiGene | Active, not recruiting ➔ Completed | Trial completion date: Nov 2025 ➔ May 2025 | Trial primary completion date: Nov 2025 ➔ May 2025

Trial completion • Trial completion date • Trial primary completion date

BGB-43395-103: A Study of Different Forms of BGB-43395 and Food Effect in Healthy Participants (clinicaltrials.gov) - P1 | N=48 | Active, not recruiting | Sponsor: BeiGene | Recruiting ➔ Active, not recruiting | Trial completion date: May 2025 ➔ Nov 2025 | Trial primary completion date: May 2025 ➔ Nov 2025

Enrollment closed • Trial completion date • Trial primary completion date

BGB-43395 Alone or as Part of Combination Therapies in Participants With Breast Cancer and Other Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=300 | Recruiting | Sponsor: BeiGene | N=79 ➔ 300 | Trial completion date: May 2026 ➔ Jun 2028 | Trial primary completion date: May 2026 ➔ Jun 2028

Enrollment change • Trial completion date • Trial primary completion date • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • HER-2

BGB-43395-102: BGB-43395 Alone or as Part of Combination Therapies in Chinese Participants With HR+/HER2- Breast Cancer and Other Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=33 | Active, not recruiting | Sponsor: BeiGene | Recruiting ➔ Active, not recruiting | N=78 ➔ 33

Enrollment change • Enrollment closed • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

BG-68501-101: A Study to Examine the Safety of Different Doses of BG-68501 Given to Participants With Advanced-Stage Tumors (clinicaltrials.gov) - P1 | N=218 | Recruiting | Sponsor: BeiGene | N=138 ➔ 218

Enrollment change • Platinum resistant • Bladder Cancer • Breast Cancer • Endometrial Cancer • Esophageal Cancer • Gastric Cancer • Gastroesophageal Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Small Cell Lung Cancer • Solid Tumor • Triple Negative Breast Cancer

BeiGene Announces Fourth Quarter and Full Year 2024 Financial Results and Business Updates (Businesswire) - "Anticipate data readouts for BGB-43395 (CDK4 inhibitor), BG-68501 (CDK2 inhibitor) and BG-C9074 (B7H4 ADC) in the first half of 2025"

Clinical data • P1 data • Oncology • Solid Tumor

BeiGene Announces Fourth Quarter and Full Year 2024 Financial Results and Business Updates (Businesswire) - "Advan-TIG-302 (TIGIT antibody): anticipate interim data readout from Phase 3 study in first-line PD(L)1-high non small cell lung cancer in the second half of 2025...BGB-43395 (CDK4 inhibitor): continued dose escalation in monotherapy and in combination with fulvestrant and letrozole in the anticipated efficacious dose range; more than 180 patients enrolled to date and proof-of-concept expected in the first half of 2025...Zanidatamab (HER2 bispecific antibody) in combination with tislelizumab and chemotherapy: anticipate primary PFS data readout from Phase 3 study in first-line HER2-positive gastroesophageal adenocarcinoma in the second half of 2025...BGB-45035 (IRAK4 CDAC): currently in dose escalation in both SAD and MAD cohorts with more than 130 subjects enrolled...Phase 2 study planned in 2025; proof-of-concept for tissue IRAK4 degradation in the second half of 2025."

Clinical data • New P2 trial • Breast Cancer • Gastroesophageal Cancer • Immunology • Non Small Cell Lung Cancer

BGB-21447 (Bcl-2 Inhibitor) Combinations for Adults With Hormone-Receptor Positive (HR+)/Human Epidermal Growth Factor Receptor 2 Negative (HER2-) Metastatic Breast Cancer (clinicaltrials.gov) - P1 | N=92 | Recruiting | Sponsor: BeiGene | Not yet recruiting ➔ Recruiting

Enrollment open • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • BCL2

BGB-43395-103: A Study of Different Forms of BGB-43395 and Food Effect in Healthy Participants (clinicaltrials.gov) - P1 | N=48 | Recruiting | Sponsor: BeiGene | Not yet recruiting ➔ Recruiting

Enrollment open

BGB-21447 (Bcl-2 Inhibitor) Combinations for Adults With Hormone-Receptor Positive (HR+)/Human Epidermal Growth Factor Receptor 2 Negative (HER2-) Metastatic Breast Cancer (clinicaltrials.gov) - P1 | N=92 | Not yet recruiting | Sponsor: BeiGene

New P1 trial • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • BCL2

A Study of Different Forms of BGB-43395 and Food Effect in Healthy Participants (clinicaltrials.gov) - P1 | N=48 | Not yet recruiting | Sponsor: BeiGene

New P1 trial

Company News丨BeiGene Announces Breast Cancer Pipeline [Google translation] (bydrug.pharmcube.com) - "Recently, BeiGene...presented for the first time at the San Antonio Breast Cancer Symposium (SABCS) and announced the latest data on the company's breast cancer treatment product portfolio. Poster presentations included first-in-human data from BeiGene's investigational cyclin-dependent kinase (CDK) 4 inhibitor BGB-43395 for the treatment of hormone receptor-positive (HR+)/human epidermal growth factor receptor 2-negative (HER2-) breast cancer patients. Two posters highlighted the ongoing trial designs for BGB-43395 and CDK2 inhibitor BG-68501/EXT-197, and one poster detailed the preclinical characteristics of BGB-43395."

P1 data • Preclinical • Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer

Preclinical characterization of BGB-43395, a potential best-in-class CDK4 selective inhibitor with potent pharmacodynamic and anti-tumor activity in HR+HER2- breast cancer models (SABCS 2024) - P1 | "In the biochemical assay, BGB-43395 exhibits superior kinase inhibition against CDK4 compared to approved CDK4/(6) inhibitors (palbociclib, ribociclib and abemaciclib) and investigational CDK4 inhibitor PF-07220060...BGB-43395 in combination with fulvestrant also demonstrated a greater tumor growth inhibition compared to palbociclib in combination with fulvestrant in HR+HER2- MCF7 xenograft models. In summary, BGB-43395 is a potential best-in-class CDK4 inhibitor with high potency and selectivity over CDK6 and other kinases, providing an opportunity to achieve high exposure and thus maximum on-target CDK4 inhibition for the treatment of HR+HER2- breast cancer and other CDK4 dependent cancers. BGB-43395 is currently undergoing clinical investigation as monotherapy or in combination with endocrine therapies in patients with metastatic HR+HER2- BC and other advanced solid tumors (NCT06120283)."

PK/PD data • Preclinical • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • HER-2 • RB1

First-in-human phase 1a, dose-escalation study of BGB-43395 (CDK4-selective inhibitor) as monotherapy and in combination with fulvestrant or letrozole in patients with metastatic HR+/HER2+ breast cancer and other advanced solid tumors (SABCS 2024) - P1 | "BGB-43395 is a novel CDK4-selective inhibitor and a promising agent for tumors with high CDK4 dependency with the potential to minimize off-target toxicity. To date, BGB-43395 has been safe and tolerable, supporting continued development. The dose-escalation phase is currently ongoing."

Clinical • Combination therapy • Metastases • Monotherapy • P1 data • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • CDKN2A • HER-2

Trial in progress: First-in-human phase 1a/1b, dose-escalation/expansion study of BGB-43395 (CDK4 selective inhibitor) as monotherapy or combination therapy in Chinese patients with metastatic HR+/HER2- breast cancer & other advanced solid tumors (SABCS 2024) - P1 | " This phase 1a/1b, open-label, multicenter study is evaluating the safety, tolerability, PK, pharmacodynamics (PD), and preliminary antitumor activity of BGB-43395 given orally as monotherapy or in combination with fulvestrant, letrozole, or other combination partners in Chinese pts with advanced or metastatic solid tumors, including HR+/HER2− BC (NCT06253195). Exploratory endpoints are overall survival and potential biomarkers associated with response. As of May 28, 2024, the study is currently enrolling pts, with five pts currently dosed in the dose-escalation phase across 12 sites in China."

Clinical • Combination therapy • Metastases • Monotherapy • P1 data • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • HER-2

BG-68501-101: A Study to Examine the Safety of Different Doses of BG-68501 Given to Participants With Advanced-Stage Tumors (clinicaltrials.gov) - P1 | N=138 | Recruiting | Sponsor: BeiGene | Trial completion date: Dec 2026 ➔ Feb 2028 | Trial primary completion date: Dec 2026 ➔ Feb 2028

Metastases • Trial completion date • Trial primary completion date • Bladder Cancer • Breast Cancer • Endometrial Cancer • Esophageal Cancer • Gastric Cancer • Genito-urinary Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Small Cell Lung Cancer • Solid Tumor • Triple Negative Breast Cancer • HER-2

BeiGene (06160)'s Class 1 new drug BGB-43395 tablets approved for clinical use in breast cancer and other solid tumors [Google translation] (Sina Corp) - "On August 22, the official website of the Center for Drug Evaluation (CDE) of the China National Medical Products Administration announced that BeiGene's...Class 1 new drug BGB-43395 tablets were approved for clinical use, and are intended to be used as a single-drug treatment or in combination with fulvestrant, letrozole or other drugs to treat advanced or metastatic HR+/HER2- breast cancer and other solid tumors...More than 60 patients have been enrolled so far, and the first data readout results of the Phase 1 trial are expected to be announced in the fourth quarter of 2024."

P1 data • Trial status • Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

BeiGene Reports First Quarter 2024 Financial Results and Business Updates (Businesswire) - "BGB-43395 (CDK4 inhibitor): Initiated fourth dose level of monotherapy, which is in the efficacious dose range with no dose limiting toxicities observed; and initiated dosing of combination with fulvestrant just over four months from first monotherapy dose. BG-68501 (CDK2 inhibitor): Initiated second dose level of monotherapy in first-in-human study, with clinical pharmacokinetics as expected and no dose limiting toxicities observed. BG-C9074 (B7H4 ADC): First patient dosed in Australia in global first-in-human Phase 1 study."

Trial status • Endometrial Cancer • Gastric Cancer • HER2 Negative Breast Cancer • Hormone Receptor Positive Breast Cancer • Non Small Cell Lung Cancer • Oncology • Ovarian Cancer • Prostate Cancer • Solid Tumor

BGB-43395-102: BGB-43395 Alone or as Part of Combination Therapies in Chinese Participants With HR+/HER2- Breast Cancer and Other Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=78 | Recruiting | Sponsor: BeiGene | Not yet recruiting ➔ Recruiting

Combination therapy • Enrollment open • Metastases • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

BGB-43395 Alone or as Part of Combination Therapies in Chinese Participants With HR+/HER2- Breast Cancer and Other Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=78 | Not yet recruiting | Sponsor: BeiGene

New P1 trial • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor

BGB-43395 Alone or as Part of Combination Therapies in Participants With Breast Cancer and Other Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=79 | Recruiting | Sponsor: BeiGene | Not yet recruiting ➔ Recruiting

Combination therapy • Enrollment open • Metastases • Trial completion date • Trial initiation date • Trial primary completion date • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • HER-2

BGB-43395 Alone or as Part of Combination Therapies in Participants With Breast Cancer and Other Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=79 | Not yet recruiting | Sponsor: BeiGene | Phase classification: P1a/1b ➔ P1

Phase classification • Breast Cancer • HER2 Breast Cancer • HER2 Negative Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • HER-2